Synthesis and anti-tumor activities of N-(aminopyridine) benzamide derivaties.
- Author:
Juan FENG
1
;
Jian-Qi LI
Author Information
1. State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Benzamides;
chemical synthesis;
chemistry;
pharmacology;
Cell Line, Tumor;
Drug Screening Assays, Antitumor;
Histone Deacetylase Inhibitors;
chemical synthesis;
chemistry;
pharmacology;
Histone Deacetylases;
metabolism;
Humans
- From:
Acta Pharmaceutica Sinica
2009;44(12):1376-1382
- CountryChina
- Language:Chinese
-
Abstract:
To explore novel histone deacetylase (HDAC) inhibitors with anti-tumor activity, on the basis of preliminary studies, sixteen N-(2-amino-4-pyridine) benzamide derivaties (class A) and sixteen N-(2-amino-3-pyridine) benzamide derivaties (class B) were designed and prepared, and their structures were confirmed by 1H NMR and HR-MS individually. The results showed that 30 target compounds except V-20 and V-21 had HDACs inhibitory activity and V -13, V -14, V -16 were equal to CI-994 at 200 micromol x L(-1) in vitro. Compounds V-30, V-31 and V-32 exhibited potent inhibitory activities on Hut78, Jurkat E6-1, A549, K562 and MDA-MB-435s.
